Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 5.4.99.7 extracted from

  • Brown, G.R.; Hollinshead, D.M.; Stokes, E.S.; Waterson, D.; Clarke, D.S.; Foubister, A.J.; Glossop, S.C.; McTaggart, F.; Mirrlees, D.J.; Smith, G.J.; Wood, R.
    A novel series of 4-piperidinopyridine and 4-piperidinopyrimidine inhibitors of 2,3-oxidosqualene cyclase-lanosterol synthase (2000), J. Med. Chem., 43, 4964-4972.
    View publication on PubMed
Search for more literature for 5.4.99.7

Inhibitors

Inhibitors Comment Organism Structure
(4-Benzenesulfonyl-piperazin-1-yl)-(3,4,5,6-tetrahydro-2H-[1,4']bipyridinyl-4-yl)-methanone IC50: 143 nM Homo sapiens
(4-Benzenesulfonyl-piperazin-1-yl)-(3,4,5,6-tetrahydro-2H-[1,4']bipyridinyl-4-yl)-methanone IC50: 326 nM Rattus norvegicus
1-(2-methyl-4-pyrimidinyl)-4-(1-(4-bromophenylsulfonyl)piperazin-4-ylcarbonyl)piperidine IC50: 112 nM Homo sapiens
1-(2-methyl-4-pyrimidinyl)-4-(1-(4-bromophenylsulfonyl)piperazin-4-ylcarbonyl)piperidine 76% inhibition at 0.001 mM, IC50: 398 nM Rattus norvegicus
1-(2-oxazolinyl)-4-(1-(4-bromophenylsulfonyl)piperazin-4-ylcarbonyl)piperidine 87% inhibition at 0.001 mM Rattus norvegicus
1-(2-pyrimidinyl)-4-(1-(4-bromophenylsulfonyl)piperazin-4-ylcarbonyl)piperidine 8% inhibition at 0.001 mM Rattus norvegicus
1-(2-thiazolinyl)-4-(1-(4-bromophenylsulfonyl)piperazin-4-ylcarbonyl)piperidine complete inhibition at 0.001 mM Rattus norvegicus
1-(4-iodophenylsulfonyl)-4-(1-(4-pyridyl)piperidon-4-ylcarbonyl)piperazine IC50: 82 nM Rattus norvegicus
1-(4-pyrimidinyl)-4-(1-(4-bromophenylsulfonyl)piperazin-4-ylcarbonyl)piperidine IC50: 37 nM Homo sapiens
1-(4-pyrimidinyl)-4-(1-(4-bromophenylsulfonyl)piperazin-4-ylcarbonyl)piperidine complete inhibition at 0.001 mM, IC50: 116 nM Rattus norvegicus
4-(4-bromobenzoyl)-1-(1-(4-pyridyl)piperidin-4-ylcarbonyl)piperazine 96% inhibition at 0.001 mM Rattus norvegicus
4-(4-bromophenylmethyl)-1-(1-(4-pyridyl)piperidin-4-ylcarbonyl)piperazine complete inhibition at 0.001 mM Rattus norvegicus
[4-(4-Bromo-benzenesulfonyl)-piperazin-1-yl]-(3,4,5,6-tetrahydro-2H-[1,4']bipyridinyl-4-yl)-methanone IC50: 161 nM Homo sapiens
[4-(4-Bromo-benzenesulfonyl)-piperazin-1-yl]-(3,4,5,6-tetrahydro-2H-[1,4']bipyridinyl-4-yl)-methanone IC50: 228 nM Rattus norvegicus
{4-[4-(4,5-Dihydro-oxazol-2-yl)-benzylidene]-piperidin-1-yl}-(4-trifluoromethyl-phenyl)-methanone IC50: 90 nM, complete inhibition at 0.001 nM Rattus norvegicus

Localization

Localization Comment Organism GeneOntology No. Textmining
microsome
-
 Rattus norvegicus
-
-

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Rattus norvegicus
-
-
-

Synonyms

Synonyms Comment Organism
OSC
-
 Homo sapiens
OSC
-
 Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000037
-
 IC50: 37 nM Homo sapiens 1-(4-pyrimidinyl)-4-(1-(4-bromophenylsulfonyl)piperazin-4-ylcarbonyl)piperidine
0.000082
-
 IC50: 82 nM Rattus norvegicus 1-(4-iodophenylsulfonyl)-4-(1-(4-pyridyl)piperidon-4-ylcarbonyl)piperazine
0.00009
-
 IC50: 90 nM, complete inhibition at 0.001 nM Rattus norvegicus {4-[4-(4,5-Dihydro-oxazol-2-yl)-benzylidene]-piperidin-1-yl}-(4-trifluoromethyl-phenyl)-methanone
0.000112
-
 IC50: 112 nM Homo sapiens 1-(2-methyl-4-pyrimidinyl)-4-(1-(4-bromophenylsulfonyl)piperazin-4-ylcarbonyl)piperidine
0.000116
-
 complete inhibition at 0.001 mM, IC50: 116 nM Rattus norvegicus 1-(4-pyrimidinyl)-4-(1-(4-bromophenylsulfonyl)piperazin-4-ylcarbonyl)piperidine
0.000143
-
 IC50: 143 nM Homo sapiens (4-Benzenesulfonyl-piperazin-1-yl)-(3,4,5,6-tetrahydro-2H-[1,4']bipyridinyl-4-yl)-methanone
0.000161
-
 IC50: 161 nM Homo sapiens [4-(4-Bromo-benzenesulfonyl)-piperazin-1-yl]-(3,4,5,6-tetrahydro-2H-[1,4']bipyridinyl-4-yl)-methanone
0.000228
-
 IC50: 228 nM Rattus norvegicus [4-(4-Bromo-benzenesulfonyl)-piperazin-1-yl]-(3,4,5,6-tetrahydro-2H-[1,4']bipyridinyl-4-yl)-methanone
0.000326
-
 IC50: 326 nM Rattus norvegicus (4-Benzenesulfonyl-piperazin-1-yl)-(3,4,5,6-tetrahydro-2H-[1,4']bipyridinyl-4-yl)-methanone
0.000398
-
 76% inhibition at 0.001 mM, IC50: 398 nM Rattus norvegicus 1-(2-methyl-4-pyrimidinyl)-4-(1-(4-bromophenylsulfonyl)piperazin-4-ylcarbonyl)piperidine